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BRK inhibitor P21d

Chemical Structure : BRK inhibitor P21d

CAS No.: 1338249-87-8

BRK inhibitor P21d (PTK6 inhibitor P21d)

Catalog No.: PC-35189Not For Human Use, Lab Use Only.

BRK inhibitor P21d is a potent, selective, cell permeable inhibitor of breast tumor kinase (Brk, PTK6) with IC50 of 30 nM, shows no inhibitory activity against Aurora B and Lck (IC50>20 uM).

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    Biological Activity

    BRK inhibitor P21d is a potent, selective, cell permeable inhibitor of breast tumor kinase (Brk, PTK6) with IC50 of 30 nM, shows no inhibitory activity against Aurora B and Lck (IC50>20 uM).
    BRK inhibitor P21d exhibits potent cellular activity with p-SAM68 IC50 of 52 nM, downregulates SNAIL protein and restores E-cadherin expression in TNBC cells.
    BRK inhibitor P21d suppresses migration of MDA-MB-231 and MMTV-myc cells, sensitizes TNBC cells to anoikis and suppresses metastasis formation.

    Physicochemical Properties

    M.Wt 447.474
    Formula C23H22FN7O2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (4-((6-cyclopropyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl)amino)-3-fluorophenyl)(morpholino)methanone

    References

    1. Zeng H, et al. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5870-5.

    2. Ito K, et al. Cancer Res. 2016 Aug 1;76(15):4406-17.

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